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Nifedipine composition capable of increasing biological availability

A nifedipine and composition technology, applied in the field of nifedipine composition, can solve the problems of low nifedipine bioavailability, low bioavailability of active ingredients, low water solubility of nifedipine, etc.

Inactive Publication Date: 2017-11-24
HEFEI HUAFANG PHARMA SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

But nifedipine water solubility is low (dissolubility is poor), causes the bioavailability of active ingredient to be low, not only there is certain difficulty in the pharmaceutical preparation of medical field, and because nifedipine bioavailability is low, cause its clinical application The curative effect in application is not ideal, and needs to be solved

Method used

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  • Nifedipine composition capable of increasing biological availability
  • Nifedipine composition capable of increasing biological availability

Examples

Experimental program
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Effect test

experiment example 1

[0029] 12 healthy Beagle dogs were selected, randomly divided into three groups, 4 dogs in each group, fed with normal group, laver (containing Fe 3+ ions) group and vitamin C group. During the test period, the Beagle dogs were fasted overnight without water (feeding deionized water) for at least 12 hours, collected venous blood, separated plasma, and used it as a 0-hour blood drug concentration sample. Then start to feed according to the experimental grouping, the normal group dogs do not feed food, the laver group dogs are fed with 100ml laver soup, and the vitamin C group dogs are fed with vitamin C tablet 0.1g (1 tablet, 0.1g / sheet). After 30 minutes, each dog was fed with 5 mg of nifedipine tablet (1 tablet, 5 mg / tablet). After administration, blood samples were collected at 0h, 1h, 1.5h, 2h, 2.5h, 3h, 4h, 5h, 6h, 8h, 10h, 12h, 24h, 48h, placed in anticoagulant tubes containing EDTA, 3000r / min After centrifugation for 10 min, the plasma was collected and stored at -20°C...

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Abstract

The invention discloses a nifedipine composition capable of increasing biological availability. The invention firstly provides a method for increasing the biological availability of nifedipine. The method comprises the following step of using the nifedipine in an effective quantity with an antioxidant or a metal ion complexing agent in a united manner. The invention further provides a medical composition using the nifedipine as an active component and capable of increasing the biological availability. The medical composition comprises the antioxidant, and the antioxidant includes but is not limited to a free radical adsorbent, a metal ion chelating agent, an oxygen scavenger, a peroxide decomposition agent or an enzyme antioxidant.

Description

technical field [0001] The invention relates to a nifedipine composition, in particular to a nifedipine composition with improved bioavailability, and belongs to the field of nifedipine preparations. Background technique [0002] Nifedipine is the first generation of calcium antagonists, known to be very effective compounds in the treatment of hypertension and coronary heart disease and other applications, and was one of the world's best-selling drugs in the mid-1980s. The characteristics of the drug are: quick onset, high peak / valley ratio, which leads to the activation of neurohumoral fluid. After years of clinical use, the curative effect of the drug has been affirmed. But nifedipine water solubility is low (dissolubility is poor), causes the bioavailability of active ingredient to be low, not only there is certain difficulty in the pharmaceutical preparation of medical field, and because nifedipine bioavailability is low, cause its clinical application The curative effe...

Claims

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Application Information

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IPC IPC(8): A61K31/4422A61K31/375A61K47/22A61K47/18A61K47/06A61K47/02A61K47/10A61K47/14A61K47/12A61K47/26A61P9/12A61P9/10
CPCA61K31/375A61K31/4422A61K47/02A61K47/06A61K47/10A61K47/12A61K47/14A61K47/183A61K47/22A61K47/26A61K2300/00
Inventor 彭扶云何勇高永好吴宗好
Owner HEFEI HUAFANG PHARMA SCI & TECH
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